Keytruda - $7.3 billion
Darzalex - $5.6 billion
Opdivo - $4.5 billion
Tagrisso - $3.2 billion
Revlimid - $3.0 billion
Verzenio - $2.4 billion
Imfinzi - $2.3 billion
Ibrance - $2.2 billion
Perjeta - $1.9 billion
Tecentriq - $1.8 billion
In the constantly evolving field of oncology, several cancer drugs have emerged as best-sellers due to their effectiveness in treating various types of cancer. Below, we explore some of the top-selling cancer drugs, detailing their FDA-approved indications, mechanisms of action, and sales figures.
1. Keytruda (Pembrolizumab) - $7.3 billion
Indications Approved by FDA:
Non-small cell lung cancer (NSCLC)
Melanoma
Head and neck squamous cell carcinoma (HNSCC)
Classical Hodgkin lymphoma
Urothelial carcinoma
Gastric cancer
Esophageal cancer
Triple-negative breast cancer (TNBC)
Renal cell carcinoma (RCC)
Microsatellite instability-high (MSI-H) cancers
Colorectal cancer
Hepatocellular carcinoma (HCC)
Cervical cancer
Mechanism of Action: Keytruda is a monoclonal antibody that targets the programmed death-1 (PD-1) receptor on T cells. By binding to PD-1, it prevents the interaction between PD-1 and its ligands, PD-L1 and PD-L2, which are often overexpressed on cancer cells. This blockade reactivates T cells, allowing them to recognize and attack cancer cells.
2. Darzalex (Daratumumab) - $5.6 billion
Indications Approved by FDA:
Multiple myeloma
Mechanism of Action: Darzalex is a monoclonal antibody that targets CD38, a glycoprotein expressed on the surface of multiple myeloma cells. By binding to CD38, Darzalex induces tumor cell death through multiple mechanisms, including complement-dependent cytotoxicity, antibody-dependent cellular cytotoxicity, and antibody-dependent cellular phagocytosis. It also modulates the immune system to attack the cancer cells.
3. Opdivo (Nivolumab) - $4.5 billion
Indications Approved by FDA:
NSCLC
Melanoma
RCC
HNSCC
Urothelial carcinoma
Classical Hodgkin lymphoma
Hepatocellular carcinoma
Esophageal squamous cell carcinoma
Gastric cancer
Colorectal cancer with MSI-H/dMMR
Small cell lung cancer (SCLC)
Mechanism of Action: Opdivo is another immune checkpoint inhibitor that targets the PD-1 receptor on T cells. Like Keytruda, it blocks the PD-1/PD-L1 interaction, enhancing the immune system's ability to recognize and destroy cancer cells.
4. Tagrisso (Osimertinib) - $3.2 billion
Indications Approved by FDA:
EGFR T790M mutation-positive NSCLC
First-line treatment of metastatic NSCLC with EGFR exon 19 deletions or exon 21 L858R mutations
Mechanism of Action: Tagrisso is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It selectively inhibits both EGFR sensitizing mutations and the T790M resistance mutation, which is a common cause of resistance to earlier-generation EGFR TKIs. By blocking these mutations, Tagrisso inhibits cancer cell proliferation and induces apoptosis.
5. Revlimid (Lenalidomide) - $3.0 billion
Indications Approved by FDA:
Multiple myeloma
Mantle cell lymphoma
Myelodysplastic syndromes (MDS)
Follicular lymphoma
Mechanism of Action: Revlimid is an immunomodulatory drug that has multiple mechanisms of action, including direct anti-proliferative effects on tumor cells, inhibition of angiogenesis, and immune system modulation. It also enhances T-cell and natural killer (NK) cell-mediated cytotoxicity and reduces the production of pro-inflammatory cytokines.
6. Verzenio (Abemaciclib) - $2.4 billion
Indications Approved by FDA:
HR-positive, HER2-negative advanced or metastatic breast cancer
Mechanism of Action: Verzenio is an oral, selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting CDK4/6, Verzenio prevents the phosphorylation of the retinoblastoma protein (Rb), leading to cell cycle arrest at the G1 phase, thereby inhibiting the proliferation of cancer cells.
7. Imfinzi (Durvalumab) - $2.3 billion
Indications Approved by FDA:
Unresectable stage III NSCLC
Extensive-stage small cell lung cancer (ES-SCLC)
Urothelial carcinoma
Mechanism of Action: Imfinzi is a monoclonal antibody that targets PD-L1, a ligand for PD-1. By binding to PD-L1, Imfinzi prevents it from interacting with PD-1 on T cells, thereby restoring immune responses and allowing the immune system to attack the cancer.
8. Ibrance (Palbociclib) - $2.2 billion
Indications Approved by FDA:
HR-positive, HER2-negative advanced or metastatic breast cancer
Mechanism of Action: Ibrance is an oral CDK4/6 inhibitor, similar to Verzenio. It works by inhibiting CDK4/6, which leads to cell cycle arrest in the G1 phase. This action reduces cancer cell proliferation, particularly in HR-positive breast cancer.
9. Perjeta (Pertuzumab) - $1.9 billion
Indications Approved by FDA:
HER2-positive breast cancer
Mechanism of Action: Perjeta is a monoclonal antibody that targets the HER2 receptor, a protein that is overexpressed in some breast cancers. Perjeta binds to a different epitope on HER2 than Herceptin (trastuzumab), allowing for a more comprehensive blockade of HER2 signaling. This dual inhibition results in a more potent suppression of tumor growth.
10. Tecentriq (Atezolizumab) - $1.8 billion
Indications Approved by FDA:
NSCLC
SCLC
Urothelial carcinoma
Triple-negative breast cancer (TNBC)
Hepatocellular carcinoma (HCC)
Mechanism of Action: Tecentriq is a monoclonal antibody that targets PD-L1, similar to Imfinzi. By blocking the PD-L1/PD-1 interaction, Tecentriq reactivates T cells to detect and destroy cancer cells.
留言